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- Title
Strong Antibiotic Activity of the Myxocoumarin Scaffold in vitro and in vivo.
- Authors
Hertrampf, Gesa; Kusserow, Kalina; Vojnovic, Sandra; Pavic, Aleksandar; Müller, Jonas I.; Nikodinovic‐Runic, Jasmina; Gulder, Tobias A. M.
- Abstract
The increasing emergence of resistances against established antibiotics is a substantial threat to human health. The discovery of new compounds with potent antibiotic activity is thus of utmost importance. Within this work, we identify strong antibiotic activity of the natural product myxocoumarin B from Stigmatella aurantiaca MYX‐030 against a range of clinically relevant bacterial pathogens, including clinical isolates of MRSA. A focused library of structural analogs was synthesized to explore initial structure‐activity relationships and to identify equipotent myxocoumarin derivatives devoid of the natural nitro substituent to significantly streamline synthetic access. The cytotoxicity of the myxocoumarins as well as their potential to cure bacterial infections in vivo was established using a zebrafish model system. Our results reveal the exceptional antibiotic activity of the myxocoumarin scaffold and hence its potential for the development of novel antibiotics.
- Subjects
COUMARINS; STRUCTURE-activity relationships; ANTIBIOTICS; NATURAL products; BACTERIAL diseases; METHICILLIN-resistant staphylococcus aureus
- Publication
Chemistry - A European Journal, 2022, Vol 28, Issue 32, p1
- ISSN
0947-6539
- Publication type
Academic Journal
- DOI
10.1002/chem.202200394